State Key Laboratory of Bioelectronics, Jiangsu Key Laboratory for Biomaterials and Devices, School of Biological Sciences & Medical Engineering, Southeast University, Nanjing, China; Collaborative Innovation Center of Suzhou Nano-Science and Technology, Suzhou Key Laboratory of Biomaterials and Technologies, Suzhou, China.
State Key Laboratory of Bioelectronics, Jiangsu Key Laboratory for Biomaterials and Devices, School of Biological Sciences & Medical Engineering, Southeast University, Nanjing, China.
J Pharm Sci. 2017 Aug;106(8):2115-2122. doi: 10.1016/j.xphs.2017.04.023. Epub 2017 Apr 26.
Iron oxide magnetic nanoparticles (MNPs) are good candidates to implement fluid therapy in critical patients in clinic integrated system. Herein, we synthesized paclitaxel (PTX)-loaded MNPs modified with methoxy polyethylene glycol (PEG)-lysine-oleic acid (PTX-MNPs-PLO), which is expected to act as a magnetic resonance imaging (MRI) contrast agent and meanwhile for cancer therapy. MNPs were synthesized by thermal decomposition. Dialysis method was applied to prepare PTX-MNPs-PLO with 3 different PEG molecular weights (1000, 2000, and 4000 Da), which were subsequently freeze-dried into powders. PTX-MNPs-PLO was characterized by transmission electron microscope, scanning electron microscope, thermogravimetric analysis, vibrating sample magnetometer, and MRI. What is more is that pharmacokinetics and distribution in vivo were processed, the results of which exhibited that PTX-MNPs-PLO had the longer circulation lifetime compared with Taxol, PTX-MNPs-PLO, and PTX-MNPs-PLO. Results of magnetic targeting in kidneys suggested that deep buried or ultrasmall magnet is likely to be more preferable. PTX-MNPs-PLO holds great promise in the application of magnetic accumulation, target drug delivery, and thermal therapy.
氧化铁磁性纳米粒子（MNPs）是将临床综合系统中的重症患者的液体疗法付诸实践的理想选择。在此，我们合成了载紫杉醇（PTX）的 MNPs，并用甲氧基聚乙二醇（PEG）-赖氨酸-油酸（PTX-MNPs-PLO）进行了修饰，有望作为磁共振成像（MRI）造影剂，同时用于癌症治疗。MNPs 通过热分解合成。采用透析法制备了 3 种不同分子量（1000、2000 和 4000 Da）的 PEG 的 PTX-MNPs-PLO，随后将其冷冻干燥成粉末。通过透射电子显微镜、扫描电子显微镜、热重分析、振动样品磁强计和 MRI 对 PTX-MNPs-PLO 进行了表征。此外，还进行了体内药代动力学和分布研究，结果表明，与紫杉醇、PTX-MNPs-PLO 和 PTX-MNPs-PLO 相比，PTX-MNPs-PLO 的循环半衰期更长。肾脏的磁靶向结果表明，深部埋藏或超小磁铁可能更具优势。PTX-MNPs-PLO 在磁积累、靶向药物输送和热疗方面具有广阔的应用前景。
